General Information of Xenobiotics (ID: XEO00380)
Xenobiotics Name
Rosiglitazone
Xenobiotics Type
Pharmaceutical Agent(s)
Classification
Approved/Marketed Drug
Structure
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3D MOL 2D MOL
PubChem CID
77999
DME(s) Modulated by This Xenobiotics
DME(s) Inhibited by This Xenobiotics
Alkaline phosphatase (ALPL) DME Info Homo sapiens [1]
Butyrylcholine esterase (BCHE) DME Info Homo sapiens [1]
Cytochrome P450 2D6 (CYP2D6) DME Info Homo sapiens [2]
Cytochrome P450 3A4 (CYP3A4) DME Info Homo sapiens [3]
DME(s) Induced by This Xenobiotics
Adenosine aminohydrolase (ADA) DME Info Homo sapiens [4]
Retinal dehydrogenase 2 (ALDH1A2) DME Info Homo sapiens [5]
Carboxylesterase 1 (CES1) DME Info Homo sapiens [6]
Cytochrome P450 1A1 (CYP1A1) DME Info Homo sapiens [7], [8]
Cytochrome P450 1A2 (CYP1A2) DME Info Homo sapiens [9]
Cytochrome P450 1B1 (CYP1B1) DME Info Homo sapiens [10]
Cytochrome P450 2B6 (CYP2B6) DME Info Homo sapiens [10]
Cytochrome P450 2C9 (CYP2C9) DME Info Homo sapiens [9]
Cytochrome P450 2J2 (CYP2J2) DME Info Homo sapiens [4]
Short-chain dehydrogenase/reductase retSDR1 (DHRS3) DME Info Homo sapiens [11]
Beta-glucuronidase (GUSB) DME Info Homo sapiens [12]
Corticosteroid 11-beta-dehydrogenase 1 (HSD11B1) DME Info Homo sapiens [4]
Quinone reductase 1 (NQO1) DME Info Homo sapiens [5], [12]
NADPH-cytochrome P450 reductase (CPR) DME Info Homo sapiens [13]
Proline dehydrogenase 1 (PRODH) DME Info Homo sapiens [14]
Superoxide dismutase 1 (SOD1) DME Info Homo sapiens [15]
Transglutaminase H (TGM2) DME Info Homo sapiens [16]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME Info Homo sapiens [9]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DME Info Homo sapiens [17]
References
1 Characterization of primary human hepatocytes, HepG2 cells, and HepaRG cells at the mRNA level and CYP activity in response to inducers and their predictivity for the detection of human hepatotoxins. Cell Biol Toxicol. 2012 Apr;28(2):69-87.
2 Evidence for triclosan-induced activation of human and rodent xenobiotic nuclear receptors. Toxicol In Vitro. 2013 Oct;27(7):2049-60.
3 The natural anthraquinones from Rheum palmatum induced the metabolic disorder of melatonin by inhibiting human CYP and SULT enzymes. Toxicol Lett. 2016 Nov 16;262:27-38.
4 Expression and inducibility of cytochrome P450s (CYP1A1, 2B6, 2E1, 3A4) in human cord blood CD34(+) stem cell-derived differentiating neuronal cells. Toxicol Sci. 2012 Oct;129(2):392-410.
5 Investigation of drug-drug interactions caused by human pregnane X receptor-mediated induction of CYP3A4 and CYP2C subfamilies in chimeric mice with a humanized liver. Drug Metab Dispos. 2012 Mar;40(3):474-80.
6 Rifampicin exacerbates isoniazid-induced toxicity in human but not in rat hepatocytes in tissue-like cultures. Br J Pharmacol. 2008 Feb;153(4):784-91.
7 Sulforaphane is not an effective antagonist of the human pregnane X-receptor in vivo. Toxicol Appl Pharmacol. 2013 Jan 1;266(1):122-31.
8 Rifampicin, a keystone inducer of drug metabolism: from Herbert Remmer's pioneering ideas to modern concepts. Drug Metab Rev. 2004 Oct;36(3-4):497-509.
9 A comprehensive evaluation of anti-diabetic drugs on nuclear receptor PXR platform. Toxicol In Vitro. 2019 Oct;60:347-358.
10 Environmental pollutants parathion, paraquat and bisphenol A show distinct effects towards nuclear receptors-mediated induction of xenobiotics-metabolizing cytochromes P450 in human hepatocytes. Toxicol Lett. 2015 Oct 1;238(1):43-53.
11 PXR induces CYP27A1 and regulates cholesterol metabolism in the intestine. J Lipid Res. 2007 Feb;48(2):373-84.
12 Comparative effects of fibrates on drug metabolizing enzymes in human hepatocytes. Pharm Res. 2005 Jan;22(1):71-8.
13 Integrated analysis of rifampicin-induced microRNA and gene expression changes in human hepatocytes. Drug Metab Pharmacokinet. 2014;29(4):333-40.
14 Essential oils of culinary herbs and spices activate PXR and induce CYP3A4 in human intestinal and hepatic in vitro models. Toxicol Lett. 2018 Oct 15;296:1-9.
15 Identification of approved drugs as potent inhibitors of pregnane X receptor activation with differential receptor interaction profiles. Arch Toxicol. 2018 Apr;92(4):1435-1451.
16 Regulation of cytochrome P450 2C9 expression in primary cultures of human hepatocytes. J Biochem Mol Toxicol. 2009 Jan-Feb;23(1):43-58.
17 Expression and transcriptional regulation of ABC transporters and cytochromes P450 in hCMEC/D3 human cerebral microvascular endothelial cells. Biochem Pharmacol. 2009 Mar 1;77(5):897-909.

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